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Protein tyrosine phosphatase (PTP) inhibitors block enzymes that remove phosphate groups from tyrosine residues. PTPs counterbalance tyrosine kinases, and the classical PTPs share a catalytic cysteine within a conserved active-site motif. Mice lacking PTP1B show increased insulin sensitivity, which made this enzyme a model target in metabolic signaling research. SHP099 and SHP394 are allosteric inhibitors of Src homology 2 domain-containing phosphatase 2 (SHP2), which relays signals from receptor tyrosine kinases. NSC 87877 acts at the catalytic sites of SHP1 and SHP2, and TCS 401 free base inhibits PTP1B. Alexidine dihydrochloride inhibits PTP localized to the mitochondrion 1 (PTPMT1), a phosphatase located in the inner mitochondrial membrane.
SHP2-IN-18 is a selective inhibitor of the SHP2 protein, exhibiting an IC50 value of 3 nM. This compound is relevant in cancer research, particularly for studying glioblastoma, as it has the potential to elucidate the role of SHP2 in tumor progression and therapeutic response. Its potent inhibition makes it a valuable tool for investigating the signaling pathways involved in malignancies associated with SHP2 dysregulation.
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TK-642 is a potent, selective inhibitor of SHP2, exhibiting an IC50 value of 2.7 nmol/L. This compound effectively suppresses the proliferation of esophageal carcinoma cells and promotes apoptosis. TK-642 serves as a valuable tool for research focused on the mechanisms of esophageal cancer and potential therapeutic strategies.
SDUY038 is an allosteric inhibitor of SHP2, demonstrating an IC50 of 1.2 μM and a KD of 0.29 μM. This compound exhibits broad antitumor activity, with IC50 values ranging from 7 to 24 μM, by effectively suppressing pERK expression. Additionally, SDUY038 has a half-life of 3.95 hours when administered orally, making it a valuable tool for studies in cancer research and signaling pathways.
RMC-3943 is an allosteric inhibitor of SHP2, demonstrating a potent inhibition of full-length SHP2 in biochemical assays with an IC50 of 2.19 nM. This compound is valuable for research into the modulation of SHP2 activity, which is implicated in various signaling pathways and disease states, including cancer. RMC-3943 can aid in elucidating the role of SHP2 in cellular processes and may contribute to the development of targeted therapies.
SHP504 is a selective inhibitor of SHP2 phosphatase, exhibiting an IC50 of 21 μM for SHP2 1–525. This compound is primarily utilized in research to investigate the role of SHP2 in various signaling pathways and cellular processes. Its inhibition capability makes SHP504 a valuable tool in studies focused on cancer, developmental biology, and autoimmune diseases, facilitating the exploration of therapeutic strategies targeting SHP2-related mechanisms.
SHP2-IN-34 is a phenyl urea derivative that acts as a selective inhibitor of the SHP2 enzyme, demonstrating promising anti-cancer activity. In preclinical studies using the CT26 mouse model, SHP2-IN-34 significantly inhibits tumor growth, highlighting its potential for innovative cancer therapies. This reagent is valuable for research applications focused on the mechanistic role of SHP2 in oncogenesis and therapeutic development against various malignancies.
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SHP2-IN-29 is a potent inhibitor of the SHP2 phosphatase, exhibiting an IC50 value of 0.18 μM. Additionally, it demonstrates inhibitory activity against PTP1B and TCPTP, with IC50 values of 4.27 μM and 4.74 μM, respectively. This compound is valuable for research applications focused on signal transduction pathways and the modulation of cellular responses in various biological contexts.
SHP2-IN-46 is an orally active inhibitor of the SHP2 enzyme, exhibiting an IC50 of 11.76 μM. This compound effectively inhibits SHP2 enzymatic activity, demonstrating significant anti-tumor properties by suppressing cell proliferation in various cancer cell lines. SHP2-IN-46 is a valuable tool for research applications related to lung adenocarcinoma, pancreatic cancer, and hepatoblastoma, facilitating investigations into the role of SHP2 in tumor biology and potential therapeutic strategies.
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SHP2-IN-31 is a specific inhibitor of the SHP2 protein phosphatase, exhibiting an IC50 of 13 nM for wild-type SHP2 while showing minimal activity against SHP1 and the SHP2 E76K mutant (>10,000 nM). This compound effectively reduces the phosphorylation of ERK in various tumor cell lines, demonstrating its potential to inhibit malignancies. Additionally, SHP2-IN-31 has been shown to suppress tumor growth in RTK/KRAS-driven xenograft models, making it a valuable tool for research into cancer therapeutics and signaling pathways.
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PTP1B-IN-4 is a non-competitive allosteric inhibitor of protein tyrosine phosphatase PTP1B, exhibiting an IC50 value of 8 μM. This compound shows promise for investigating metabolic disorders, particularly obesity and diabetes. Its mechanism of action makes it a valuable tool in the study of insulin signaling pathways and potential therapeutic strategies for related conditions.
PRL-3 Inhibitor I is a selective inhibitor of the protein tyrosine phosphatase PRL-3, exhibiting an IC50 of 0.9 μM. This compound demonstrates significant anti-invasion activity in cell-based assays, making it a valuable tool for research in cancer biology and metastasis. Its ability to modulate PRL-3 activity positions it as a candidate for further investigation in therapeutic applications targeting tumor progression and migration.
PTP Inhibitor 1 is a selective inhibitor of protein tyrosine phosphatases (PTPs), which play a crucial role in cellular signaling pathways. This compound exhibits anti-angiogenic properties, making it valuable for research related to cancer and vascular biology. PTP Inhibitor 1 can be utilized to study tumor growth, metastasis, and the regulation of angiogenesis in therapeutic contexts.
KY-226 is a potent, selective allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 0.25 μM. This compound enhances insulin and leptin signaling, demonstrating notable anti-diabetic and anti-obesity effects. Additionally, KY-226 offers neuroprotective properties, safeguarding neurons from cerebral ischemic injury, making it a valuable tool for research into metabolic disorders and neuroprotection.
Diorcinol is a potent inhibitor of Src homology region 2 domain-containing phosphatase-1 (SHP1), exhibiting an IC50 of 0.96 μM. Isolated from Aspergillus sydowii, Diorcinol demonstrates effective blood-brain barrier penetration. This compound is valuable for research applications focused on diabetes and related metabolic disorders, as well as studies involving the modulation of immune responses.
CPT-157633 is a potent PTP1B inhibitor that functions by blocking the activity of protein tyrosine phosphatase 1B. This compound has demonstrated the ability to prevent glucose intolerance associated with binge drinking, making it relevant for research in metabolic disorders and alcohol-related conditions. Its specific mechanism of action allows for further exploration in the context of diabetes and insulin sensitivity studies.
Uralenol is a natural inhibitor of protein tyrosine phosphatase 1B (PTP1B), exhibiting an IC50 of 21.5 μM. PTP1B is critically involved in the dephosphorylation of the insulin receptor, making Uralenol a valuable compound for studies focused on insulin signaling and metabolic regulation. Its application in biochemical research can elucidate the role of PTP1B in insulin resistance and diabetes-related pathways.
2-Bromo-4'-hydroxyacetophenone functions as a potent inhibitor of PTP1B, exhibiting a Ki value of 42 μM. This compound serves as an important intermediate in the synthesis of LXRα/β antagonists. Additionally, 2-Bromo-4'-hydroxyacetophenone is utilized in research focused on hematological diseases, providing valuable insights into therapeutic pathways. Its distinctive chemical properties make it a useful tool for investigating various biological processes.
cis-Ferulic acid 4-O-β-D-glucopyranoside is a phenolic glycoside that selectively inhibits Protein Tyrosine Phosphatase 1B (PTP1B). This compound demonstrates significant antioxidant activity and plays a critical role in the modulation of cellular signaling pathways. It is relevant for research applications focused on diabetes, obesity, and metabolic syndrome, providing insights into therapeutic mechanisms involving PTP1B inhibition.
Kaempferol-7,4'-dimethyl ether is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B), demonstrating an IC50 value of 16.92 μM. It exhibits a significant inhibition rate of 46.1% at a concentration of 100 μM, and additionally, it has been shown to inhibit nitric oxide (NO) production. This compound is valuable for research applications focusing on metabolic disorders, obesity, and diabetes, where PTP1B plays a critical role in insulin signaling.
PTP1B-IN-15 is a potent and selective inhibitor of protein tyrosine phosphatase 1B (PTP1B), an enzyme involved in regulating insulin signaling and energy homeostasis. This compound demonstrates significant biological activity in modulating glucose metabolism and has potential applications in researching type II diabetes and obesity. Its specificity for PTP1B makes it a valuable tool for elucidating the role of this phosphatase in metabolic disorders.
PTP1B-IN-22 is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B), a key regulator of insulin signaling. This compound enhances glucose uptake in skeletal muscle L6 myotubes, making it a valuable tool for studying metabolic pathways and insulin resistance. It can be utilized in research addressing obesity, diabetes, and related metabolic disorders.
(4-Phenylphenoxy)phosphonic acid is an inhibitor of protein tyrosine phosphatases (PTPs), exhibiting a Km value of 86 μM. This compound is instrumental for studies exploring the role of PTPs in various biological processes, including their implications in tuberculosis research. Its ability to modulate phosphatase activity makes it a valuable tool for understanding signal transduction pathways and potential therapeutic targets in infectious diseases.
DPM-1003 is a potent PTP1B conformational inhibitor that specifically targets the non-catalytic disordered segment at the C-terminus of the PTP1B protein. This compound has demonstrated significant efficacy in reducing lung inflammation in murine models, highlighting its potential for therapeutic applications in inflammatory diseases. DPM-1003 serves as a valuable tool for researchers investigating the role of PTP1B in various biological processes and disease states.
PRL-3 Inhibitor 2 is a selective inhibitor of the protein tyrosine phosphatase PRL-3, demonstrating an IC50 of 28.1 µM. This compound exhibits significant biological activity in modulating cell signaling pathways associated with cancer progression and metastasis. It serves as a valuable tool in cancer research, particularly in studies investigating the role of PRL-3 in tumor growth and development.
ML 400 is a selective inhibitor of lipid metabolism protein tyrosine phosphatase (LMPTP), exhibiting an IC50 value of 1680 nM. This compound has been shown to effectively inhibit adipogenesis, making it a valuable tool for research in metabolic disorders and obesity studies. ML 400's specificity for LMPTP positions it as a crucial reagent for investigating the molecular mechanisms underlying lipid metabolism and related diseases.
